TAAR1 Agonist | Rat TAAR1 | Mouse TAAR1 | Human TAAR1 | ||||||
---|---|---|---|---|---|---|---|---|---|
EC50 | Efficacy | Ki | EC50 | Efficacy | Ki | EC50 | Efficacy | Ki | |
Endogenous ligands | |||||||||
PEAa | 0.11 | 100 | 0.24 | 0.20 | 102 | 0.31 | 0.26 | 104 | |
TYRa | 0.030 | 94 | 0.059 | 0.28 | 88 | 0.38 | 0.99 | 91 | |
TRPa | 0.41 | 91 | 0.13 | 2.7 | 117 | 1.4 | 21 | 73 | |
Octopamineb | 2.1 | 100 | 20 | 100 | 10 | 100 | |||
Dopamineb | 5.1 | 50 | 12 | 50 | 16 | 50 | |||
Serotoninb | 5.2 | 50 | >50 | >50 | 100 | ||||
3-MTc | 0.70 | ||||||||
Amphetamine likea | |||||||||
Amphetamine | 0.66 | 91 | 0.23 | 0.53 | 90 | 0.089 | 2.8 | 91 | |
4-fluoroamphetamine | 0.069 | 78 | 0.081 | 0.13 | 77 | 0.32 | 3.5 | 67 | |
4-methylamphetamine | 0.11 | 93 | 0.10 | 0.071 | 94 | 0.15 | >30 | ||
Methamphetamine | 0.85 | 73 | 0.35 | 0.73 | 78 | 0.55 | 5.3 | 70 | |
4-fluoromethamphetamine | 0.16 | 76 | 0.24 | 0.46 | 69 | 1.7 | 6.2 | 44 | |
MDMA | 1.0 | 56 | 0.37 | 4.0 | 71 | 2.4 | 35 | 26 | |
MDA | 0.74 | 86 | 0.25 | 0.58 | 102 | 0.16 | 3.6 | 11 | |
Cathinone | 1.2 | 28 | 2.2 | 1.2 | 66 | 2.1 | 6.9 | 53 | |
Methcathinone | 8.2 | 41 | 4.1 | 6.8 | 64 | >10 | >30 | ||
Benzofuransa | |||||||||
4-(2-aminopropyl)benzofuran (4-APB) | 0.16 | 75 | 0.11 | 0.85 | 72 | 2.1 | 4.1 | 50 | |
5-(2-aminopropyl)benzofuran (5-APB) | 0.067 | 88 | 0.042 | 0.13 | 67 | 0.11 | 6.1 | 43 | |
6-(2-aminopropyl)benzofuran (6-APB) | 0.042 | 90 | 0.052 | 0.067 | 93 | 0.056 | 7.2 | 47 | |
7-(2-aminopropyl)benzofuran (7-APB) | 0.058 | 109 | 0.066 | 0.11 | 95 | 0.13 | 0.63 | 89 | |
6-aminopropyl-2,3-dihydrobenzofuran (6-APDB) | 1.0 | 83 | 1.0 | 0.51 | 95 | 0.21 | >10 | ||
Phenethylaminesa | |||||||||
2,5-dimethoxy-4-bromo-phenethylamine (2C-B) | 0.24 | 57 | 0.079 | 2.3 | 69 | 2.2 | 3.3 | 10 | |
8-bromo-2,3,6,7-benzodihydro-difuran-ethylamine (2C-B-Fly) | 0.27 | 48 | 0.029 | 1.8 | 49 | 0.71 | >30 | ||
4-ethyl-2,5-dimethoxyphenethylamine (2C-E) | 0.18 | 72 | 0.066 | 1.1 | 64 | 1.2 | >10 | ||
2,5-dimethoxyphenethylamine (2C-H) | 1.5 | 80 | 0.90 | 7.5 | 56 | 11 | 6.5 | 53 | |
2,5-dimethoxy-4-propyl-phenethylamine (2C-P) | 0.030 | 84 | 0.020 | 0.56 | 91 | 0.28 | 4.2 | 72 | |
Mescaline | 3.7 | 37 | 3.3 | 4.8 | 25 | 11 | >10 | ||
(−)-Ephedrine | 2.5 | 42 | 3.7 | 14 | 31 | >15 | >10 | ||
4-thio-substituted phenethylaminesd | |||||||||
2C-T-3 | 0.0080 | 0.47 | >30 | ||||||
2C-T-7 (“blue mystic”) | 0.010 | 0.31 | >30 | ||||||
2C-T-19 | 0.0048 | 0.096 | >30 | ||||||
2C-T-31 | 0.0052 | 0.055 | >30 | ||||||
TRPsa | |||||||||
Psilocin | 0.92 | 85 | 1.4 | 2.7 | 80 | 17 | >30 | ||
DMT | 1.5 | 81 | 2.2 | 1.2 | 73 | 3.3 | >10 | ||
Ergolines | |||||||||
Lysergic acid diethylamide (LSD)a | 1.4 | 29 | 0.45 | 9.7 | 13 | 10 | >20 | ||
Piperazinesa | |||||||||
m-Chlorophenylpiperazine (m-CPP) | 0.15 | 60 | 0.054 | 3.2 | 40 | 6.6 | >30 | ||
Trifluoromethylphenylpiperazine (TFMPP) | 0.75 | 59 | 0.38 | 3.8 | 44 | 2.3 | >30 | ||
Aminoindanesa | |||||||||
2-aminoindane (2-AI) | 0.11 | 90 | 0.31 | 0.33 | 54 | 2.1 | 1.5 | 110 | |
N-methyl-2-AI | 0.37 | 63 | 0.53 | 0.94 | 108 | 2.6 | 3.3 | 54 | |
5-iodo-2-aminoindane (5-IAI) | 0.033 | 96 | 0.030 | 0.41 | 36 | 1.1 | 3.2 | 33 | |
5,6-methylenedioxy-2-aminoindane (MDAI) | 0.22 | 95 | 0.57 | 0.52 | 99 | 1.8 | 4.1 | 30 | |
Miscellaneous nonselective compounds | |||||||||
Apomorphinee | 0.99 | 79 | 0.37 | 2.5 | 59 | 0.37 | >20 | 0.70 | |
Ractopaminef | 0.016 | 100 | |||||||
3ITg,h | 0.014 | 0.090 | 61 | 1.7 | 56 | ||||
Clonidinei | 0.21 | 0.97 | |||||||
Guanabenzi | 0.007 | 0.025 | |||||||
Idazoxani | 0.11 | 6.7 | |||||||
Selective compounds | |||||||||
RO5073012j | 0.025 | 24 | 0.0011 | 0.023 | 26 | 0.0032 | 0.025 | 34 | 0.0058 |
RO5166017k | 0.014 | 90 | 0.0027 | 0.0033 | 65 | 0.0019 | 0.055 | 95 | 0.031 |
RO5203648l | 0.0068 | 59 | 0.0010 | 0.0040 | 48 | 0.0005 | 0.030 | 73 | 0.0068 |
RO5256390m | 0.0051 | 107 | 0.0029 | 0.0020 | 79 | 0.0044 | 0.016 | 98 | 0.024 |
RO5263397m | 0.047 | 76 | 0.0091 | 0.0013 | 59 | 0.0009 | 0.017 | 81 | 0.0041 |
Selective inverse agonist | |||||||||
RO5212773 (EPPTB)n | 4.5 | 0 | 0.94 | 0.028 | −12 | 0.0009 | 7.5 | 0 | >5.0 |
↵a Simmler et al. (2016).
↵b Lindemann et al. (2005).
↵c Sotnikova et al. (2010).
↵d Luethi et al. (2017).
↵e Sukhanov et al. (2014).
↵f Liu et al. (2014).
↵g Scanlan et al. (2004).
↵h Coster et al. (2015).
↵i Hu et al. (2009).
↵j Revel et al. (2012a).
↵k Revel et al. (2011).
↵l Revel et al. (2012b).
↵m Revel et al. (2013).
↵n Stalder et al. (2011). IC50 values are presented in lieu of EC50 values.